Abstract
Histone deacetylases (HDACs) are key enzymes in the regulation of gene expression. By maintaining the dynamic equilibrium of the acetylation status of highly conserved lysine residues on histones, they regulate chromatin remodeling and gene expression. A link between aberrant HDAC activity and cancer has been widely reported and HDAC inhibitors have been shown to inhibit the proliferation of human tumor cell lines in vitro. Furthermore, several HDAC inhibitors have exhibited potent anti-tumor activity in human xenograft models, suggesting this class of compounds to be promising novel cancer therapeutic agents. This review provides an update on the current knowledge of HDAC inhibition with a focus on the most recent progress of HDAC inhibitors in clinical development.
Keywords: chromatin, histone acetylation, anti-cancer
Current Medicinal Chemistry
Title: Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics
Volume: 10 Issue: 22
Author(s): Janine Arts, Stefanie de Schepper and Kristof Van Emelen
Affiliation:
Keywords: chromatin, histone acetylation, anti-cancer
Abstract: Histone deacetylases (HDACs) are key enzymes in the regulation of gene expression. By maintaining the dynamic equilibrium of the acetylation status of highly conserved lysine residues on histones, they regulate chromatin remodeling and gene expression. A link between aberrant HDAC activity and cancer has been widely reported and HDAC inhibitors have been shown to inhibit the proliferation of human tumor cell lines in vitro. Furthermore, several HDAC inhibitors have exhibited potent anti-tumor activity in human xenograft models, suggesting this class of compounds to be promising novel cancer therapeutic agents. This review provides an update on the current knowledge of HDAC inhibition with a focus on the most recent progress of HDAC inhibitors in clinical development.
Export Options
About this article
Cite this article as:
Arts Janine, Schepper de Stefanie and Emelen Van Kristof, Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics, Current Medicinal Chemistry 2003; 10 (22) . https://dx.doi.org/10.2174/0929867033456657
DOI https://dx.doi.org/10.2174/0929867033456657 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Recent Trends in Tubulin-Binding Combretastatin A-4 Analogs for
Anticancer Drug Development
Current Medicinal Chemistry <i>In Vitro</i> Cytotoxicity and Apoptosis Inducing Evaluation of Novel Halogenated Isatin Derivatives
Anti-Cancer Agents in Medicinal Chemistry Structure-Function Relationships of PEDF
Current Molecular Medicine Genetic Factors in Parkinsons Disease and Potential Therapeutic Targets
Current Neuropharmacology HIF-1α and Calcium Signaling as Targets for Treatment of Prostate Cancer by Cardiac Glycosides
Current Cancer Drug Targets Mechanism of Cancer Drug Resistance and the Involvement of Noncoding RNAs
Current Medicinal Chemistry GSK-3 Inhibitors as New Leads to Treat Type-II Diabetes
Current Drug Targets Compartmentalized Platforms for Neuro-Pharmacological Research
Current Neuropharmacology Targeting Aurora Kinases in Cancer Treatment
Current Drug Targets Anti-Cancer Cytotoxic Effects of Multiwalled Carbon Nanotubes
Current Pharmaceutical Design Prolyl Oligopeptidase: A Rising Star on the Stage of Neuroinflammation Research
CNS & Neurological Disorders - Drug Targets Moving Beyond Tyrosine Hydroxylase to Define Dopaminergic Neurons for Use in Cell Replacement Therapies for Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets Dendritic Cells in Innate Immune Responses Against HIV
Current Molecular Medicine Pharmacological Profile and Pharmacogenomics of Anti-Cancer Drugs Used for Targeted Therapy
Current Cancer Drug Targets Epigenetic control of cardiovascular health by nutritional polyphenols involves multiple chromatin-modifying writer-reader-eraser proteins
Current Topics in Medicinal Chemistry Prospective Teratology of Retinoic Acid Metabolic Blocking Agents (RAMBAs) and Loss of CYP26 Activity
Current Pharmaceutical Design Is the Modulation of Autophagy the Future in the Treatment of Neurodegenerative Diseases?
Current Topics in Medicinal Chemistry Artificial Intelligence, Big Data and Machine Learning Approaches in Precision Medicine & Drug Discovery
Current Drug Targets Metabolism and the Paradoxical Effects of Arsenic: Carcinogenesis and Anticancer
Current Medicinal Chemistry 4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls
Letters in Drug Design & Discovery